The DOI matches its Crossref record; 58 of the 58 references it cites were found in a registry or an index.
Conformational Restriction: An Effective Tactic in ‘Follow-On’-Based Drug Discovery
Abstract
The conformational restriction (rigidification) of a flexible ligand has often been a commonly used strategy in drug design, as it can minimize the entropic loss associated with the ligand adopting a preferred conformation for binding, which leads to enhanced potency for a given physiological target, improved selectivity for isoforms and reduced the possibility of drug metabolism. Therefore, the application of conformational restriction strategy is a core aspect of drug discovery and development that is widely practiced by medicinal chemists either deliberately or subliminally. The present review will highlight current representative examples and a brief overview on the rational design of conformationally restricted agents as well as discuss its advantages over the flexible counterparts.
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Ostacolo, C., Miceli, F., Di Sarno, V., Nappi, P., Iraci, N., Soldovieri, M. V., Ciaglia, T., Ambrosino, P., Vestuto, V., Lauritano, A., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00796 · Cited by 39
Metadata
- Authors
- Fang, Z., Song, Y., Zhan, P., Zhang, Q., & Liu, X.
- Venue
- Future Medicinal Chemistry
- Publisher
- Informa UK Limited
- Published
- 2014-05
- Volume
- 6
- Issue
- 8
- Pages
- 885-901
- ISSN
- 1756-8919 (ISSN-L)
- 1756-8927
- OpenAlex
- W2071358460
- Cited by
- 268
- References
- 58
- FWCI
- 2.92
- Type
- journal article
- Language
- en
- Open access
- closed
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- Fang, Z., Song, Y., Zhan, P., Zhang, Q., & Liu, X. (2014). Conformational Restriction: An Effective Tactic in ‘Follow-On’-Based Drug Discovery. Future Medicinal Chemistry. https://doi.org/10.4155/fmc.14.50
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